Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2

3-bromo-5-phenyl Salicylic Acid – 25 mg

Brand:
Cayman
CAS:
4906-68-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The aldo-keto reductase (AKR) enzymes constitute a family of related NADPH-dependent oxidoreductases. The 1C subfamily (AKR1C) includes four human hydroxysteroid dehydrogenases, with AKR1C1 being a 20α-HSD and the other three being 3α-HSDs. AKR1C1 metabolizes progesterone to an inactive progestin, 20α-hydroxy progesterone.{17634} In addition, AKR1C1 actions have been implicated in cancer and in the processing of neuroactive steroids involved in brain function.{17637,17636,17638,17635} 3-bromo-5-phenyl Salicylic acid selectively inhibits AKR1C1 (Ki = 4 nM) over AKR1C2 (Ki = 87 nM), AKR1C3 (Ki = 4.2 μM), and AKR1C4 (Ki = 18.2 μM).{17245} Moreover, it potently inhibits the metabolism of progesterone by bovine aortic endothelial cells overexpressing AKR1C1 (IC50 = 460 nM).{17245}  

 

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Description

Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 4 nM) versus AKR1C2, AKR1C3, and AKR1C4 (Ki = 0.087, 4.2, and 18.2 μM, respectively); potently inhibits the metabolism of progesterone in endothelial cells overexpressing AKR1C1 (IC50 = 460 nM)

Formal name: 5-bromo-4-hydroxy-[1,1′-biphenyl]-3-carboxylic acid

Synonyms:  NSC 109116

Molecular weight: 293.1

CAS: 4906-68-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Sterol Biosynthesis||Research Area

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